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Pyridazine derivatives and their use as therapeutic agents for the treatment of skin disorders
专利权人:
ЗИНОН ФАРМАСЬЮТИКЛЗ ИНК. (CA);НОВАРТИС АГ (CH)
发明人:
БИЛЛИХ Андреас (AT),УИНТЕР Майкл Д. (CA),ГОЛДБЕРГ Йигал Пол (CA),ВИНЦЕНБУРГ Гезине (CH),РАПП Карин (CH),ФРИТЦЕ Андреас (CH)
申请号:
RU2010139285/15
公开号:
RU2010139285A
申请日:
2009.02.19
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. A method of treating a skin disorder mediated by stearoyl-CoA desaturase (SCD) in a mammal, which comprises administering to a mammal in need thereof a therapeutically effective amount of a compound of formula (I):! ! where x and y are each independently 1, 2 or 3; ! W represents —C (O) N (R1) -, —C (O) N [C (O) R1a] -, —N (R1) C (O) N (R1) -, or —N (R1) C (O) -; ! V represents —C (O) -, —C (S) - or —C (R10) H; ! each R1 is independently selected from the group consisting of hydrogen; C1-C6 alkyl optionally substituted with one or more substituents selected from the group consisting of halogen, methyl or trifluoromethyl; and C2-C6 alkyl optionally substituted with one or more substituents selected from the group consisting of methoxy and hydroxyl; ! R1a is selected from the group consisting of hydrogen, C1-C6 alkyl and cycloalkyl; ! R2 is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, C2-C12 hydroxyalkyl, C2-C12 hydroxyalkenyl, C1-C12 alkoxy, C2-C12 alkoxyalkyl, C3-C12 cycloalkyl, C1-4alkyl, acylalkyl -C12 heterocyclylalkyl, C1-C12 heteroaryl and C3-C12 heteroarylalkyl; ! or R2 is a multi-ring structure containing 2-4 rings, wherein the rings are independently selected from the group consisting of cycloalkyl, heterocyclyl, aryl and heteroaryl, and where some or all of the rings may be fused to each other; ! R3 is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, C2-C12 hydroxyalkyl, C2-C12 hydroxyalkenyl, C1-C12 alkoxy, C2-C12 alkoxyalkyl, C3-C12 cycloalkyl, C4-C12 cycloalkylalkylalkyl -C12 heterocyclylalkyl, C1-C12 heteroaryl and C3-C12 heteroarylalkyl; ! or R3 n1. Способ лечения кожного нарушения, опосредованного стеароил-CoA десатуразой (SCD) у млекопитающего, который включает введение млекопитающему, нуждающемуся в этом, терапевтически эффективного количества соединения формулы (I): ! ! где x и y каждый независимо обозначает 1, 2 или 3; ! W представляет собой -C(O)N(R1)-, -С(O)N[C(О)R1a]-, -N(R1)C(O)N(R1)- или -N(R
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